AR066063A1 - TRIAZOL DERIVATIVES THAT ARE SMO ANTAGONISTS - Google Patents
TRIAZOL DERIVATIVES THAT ARE SMO ANTAGONISTSInfo
- Publication number
- AR066063A1 AR066063A1 ARP080101540A ARP080101540A AR066063A1 AR 066063 A1 AR066063 A1 AR 066063A1 AR P080101540 A ARP080101540 A AR P080101540A AR P080101540 A ARP080101540 A AR P080101540A AR 066063 A1 AR066063 A1 AR 066063A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- solvate
- pharmaceutically acceptable
- acceptable salt
- cancer
- Prior art date
Links
- QWENRTYMTSOGBR-UHFFFAOYSA-N 1H-1,2,3-Triazole Chemical class C=1C=NNN=1 QWENRTYMTSOGBR-UHFFFAOYSA-N 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000001153 fluoro group Chemical group F* 0.000 abstract 4
- 206010028980 Neoplasm Diseases 0.000 abstract 3
- 201000011510 cancer Diseases 0.000 abstract 3
- 229910052731 fluorine Chemical group 0.000 abstract 3
- 238000000034 method Methods 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 239000012453 solvate Substances 0.000 abstract 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 230000002265 prevention Effects 0.000 abstract 2
- 230000008485 antagonism Effects 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 239000006114 chemosensitizer Substances 0.000 abstract 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 239000002534 radiation-sensitizing agent Substances 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4245—Oxadiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente proporciona un procedimiento para el tratamiento o la prevencion de dolencias que se pueden mejorar mediante antagonismo de Smo, cuyo procedimiento comprende administracion a un paciente necesitado del mismo de una cantidad eficaz de uncompuesto de formula 1 o una composicion que comprende un compuesto de formula 1, o una sal o solvato del mismo farmacéuticamente aceptable, en el que: 2 de X, Y y Z representan átomos de nitrogeno, y el otro representa un átomo de oxígeno; R1 y R2se toman conjuntamente con el átomo al que están unidos y representan un anillo ciclobutilo, opcionalmente sustituido con 1-2 átomos de fluor, y R3 representa hidrogeno o un átomo de fluor; o R1 representa metilo, R2 representa metilo o un átomo defluor y R3 representa un átomo de fluor. Reivindicacion 9: El procedimiento de cualquier reivindicacion previa en el que la dolencia es cáncer. Reivindicacion 11: El uso de un compuesto como se define en una cualquiera de las reivindicaciones 1a 8, o una sal o solvato del mismo farmacéuticamente aceptable, como quimio- o radio- sensibilizador para tratamiento del cáncer. Reivindicacion 12: Un compuesto de una cualquiera de las reivindicaciones 1 a 8, o una sal o solvato del mismofarmacéuticamente aceptable, para uso en el tratamiento o la prevencion del cáncer.This provides a procedure for the treatment or prevention of ailments that can be improved by Smo antagonism, which procedure comprises administering to a patient in need thereof an effective amount of a compound of formula 1 or a composition comprising a compound of formula 1, or a pharmaceutically acceptable salt or solvate thereof, in which: 2 of X, Y and Z represent nitrogen atoms, and the other represents an oxygen atom; R1 and R2 are taken together with the atom to which they are attached and represent a cyclobutyl ring, optionally substituted with 1-2 fluorine atoms, and R3 represents hydrogen or a fluorine atom; or R 1 represents methyl, R 2 represents methyl or a fluorine atom and R 3 represents a fluorine atom. Claim 9: The procedure of any previous claim in which the condition is cancer. Claim 11: The use of a compound as defined in any one of claims 1 to 8, or a pharmaceutically acceptable salt or solvate thereof, as a chemo- or radio sensitizer for cancer treatment. Claim 12: A compound of any one of claims 1 to 8, or a pharmaceutically acceptable salt or solvate thereof, for use in the treatment or prevention of cancer.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US92501807P | 2007-04-18 | 2007-04-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR066063A1 true AR066063A1 (en) | 2009-07-22 |
Family
ID=39433852
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080101540A AR066063A1 (en) | 2007-04-18 | 2008-04-15 | TRIAZOL DERIVATIVES THAT ARE SMO ANTAGONISTS |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US7691887B2 (en) |
| EP (1) | EP2136803B1 (en) |
| JP (1) | JP5498936B2 (en) |
| CN (1) | CN101663033B (en) |
| AR (1) | AR066063A1 (en) |
| AT (1) | ATE555785T1 (en) |
| AU (1) | AU2008241527B2 (en) |
| CA (1) | CA2683946C (en) |
| CL (1) | CL2008001074A1 (en) |
| PE (1) | PE20090806A1 (en) |
| TW (1) | TW200901987A (en) |
| WO (1) | WO2008130552A1 (en) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI433674B (en) | 2006-12-28 | 2014-04-11 | Infinity Discovery Inc | Cyclopamine analogs |
| AU2008345151A1 (en) * | 2007-12-27 | 2009-07-09 | Infinity Pharmaceuticals, Inc. | Therapeutic cancer treatments |
| US20100297118A1 (en) * | 2007-12-27 | 2010-11-25 | Macdougall John | Therapeutic Cancer Treatments |
| CA2710858A1 (en) | 2007-12-27 | 2009-07-09 | Infinity Pharmaceuticals, Inc. | Methods for stereoselective reduction |
| GB0813740D0 (en) * | 2008-07-28 | 2008-09-03 | Angeletti P Ist Richerche Biologica | Therapeutic compounds |
| EP2334683B1 (en) * | 2008-08-29 | 2017-03-22 | MSD Italia S.r.l. | Saturated bicyclic heterocyclic derivatives as smo antagonists |
| ES2567134T3 (en) | 2009-08-05 | 2016-04-20 | Infinity Pharmaceuticals, Inc. | Enzymatic transamination of cyclopamine analogs |
| WO2011063309A1 (en) * | 2009-11-20 | 2011-05-26 | Infinity Pharmaceuticals, Inc. | Methods and compositions for treating hedgehog-associated cancers |
| WO2012037217A1 (en) | 2010-09-14 | 2012-03-22 | Infinity Pharmaceuticals, Inc. | Transfer hydrogenation of cyclopamine analogs |
| EP2983674A4 (en) | 2013-04-08 | 2017-05-10 | Dennis M. Brown | Therapeutic benefit of suboptimally administered chemical compounds |
| CN104324039A (en) * | 2014-10-20 | 2015-02-04 | 付茜 | Medicine for treating lipomyoma on surface of human body and using method |
| HK1253345A1 (en) | 2015-06-04 | 2019-06-14 | Pellepharm Inc. | Topical formulations for delivery of hedgehog inhibitor compounds and use thereof |
| CN108623446A (en) * | 2017-03-24 | 2018-10-09 | 北京艾德旺科技发展有限公司 | A kind of method of synthesis 3,3- difluoro cyclobutane formates |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7291626B1 (en) | 1998-04-09 | 2007-11-06 | John Hopkins University School Of Medicine | Inhibitors of hedgehog signaling pathways, compositions and uses related thereto |
| EP1474139B1 (en) | 2002-02-01 | 2007-11-21 | Merck & Co., Inc. | 11-beta-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia |
| JO2397B1 (en) | 2002-12-20 | 2007-06-17 | ميرك شارب اند دوم كوربوريشن | Triazole Derivatives As Inhibitors Of 11-Beta -Hydroxysteriod Dehydrogenase-1 |
| DE602004028473D1 (en) | 2003-05-29 | 2010-09-16 | Merck Sharp & Dohme | TRIAZONE DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE-1 |
| WO2005033288A2 (en) | 2003-09-29 | 2005-04-14 | The Johns Hopkins University | Hedgehog pathway antagonists |
| AU2005325267B2 (en) | 2004-04-30 | 2010-11-04 | Curis Inc. | Quinoxaline inhibitors of the hedgehog signalling pathway |
| WO2006017542A1 (en) | 2004-08-06 | 2006-02-16 | Merck & Co., Inc. | Sulfonyl compounds as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1 |
| ES2578728T3 (en) | 2004-08-27 | 2016-07-29 | Infinity Pharmaceuticals, Inc. | Process for the preparation of cyclopamine analogs |
| CN102964294A (en) | 2004-09-02 | 2013-03-13 | 遗传技术研究公司 | Pyridyl inhibitors of hedgehog signalling |
| CA2583812A1 (en) | 2004-10-28 | 2006-05-11 | Irm Llc | Compounds and compositions as hedgehog pathway modulators |
| AU2005301962B2 (en) | 2004-11-03 | 2011-10-20 | Curis, Inc. | Mediators of hedgehog signaling pathways, compositions and uses related thereto |
| KR20080059236A (en) | 2005-10-20 | 2008-06-26 | 머크 앤드 캄파니 인코포레이티드 | Triazole Derivatives as Inhibitors of 11-beta-hydroxysteroid Dehydrogenase-1 |
-
2008
- 2008-04-15 US US12/082,933 patent/US7691887B2/en active Active
- 2008-04-15 WO PCT/US2008/004862 patent/WO2008130552A1/en not_active Ceased
- 2008-04-15 CL CL2008001074A patent/CL2008001074A1/en unknown
- 2008-04-15 TW TW097113665A patent/TW200901987A/en unknown
- 2008-04-15 EP EP08742913A patent/EP2136803B1/en active Active
- 2008-04-15 CN CN2008800127274A patent/CN101663033B/en active Active
- 2008-04-15 AT AT08742913T patent/ATE555785T1/en active
- 2008-04-15 JP JP2010504069A patent/JP5498936B2/en active Active
- 2008-04-15 AU AU2008241527A patent/AU2008241527B2/en active Active
- 2008-04-15 PE PE2008000654A patent/PE20090806A1/en not_active Application Discontinuation
- 2008-04-15 AR ARP080101540A patent/AR066063A1/en unknown
- 2008-04-15 CA CA2683946A patent/CA2683946C/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| PE20090806A1 (en) | 2009-06-27 |
| US20080262051A1 (en) | 2008-10-23 |
| CL2008001074A1 (en) | 2009-06-05 |
| CA2683946A1 (en) | 2008-10-30 |
| AU2008241527A1 (en) | 2008-10-30 |
| ATE555785T1 (en) | 2012-05-15 |
| JP2010524937A (en) | 2010-07-22 |
| AU2008241527B2 (en) | 2014-02-13 |
| TW200901987A (en) | 2009-01-16 |
| CN101663033A (en) | 2010-03-03 |
| CA2683946C (en) | 2013-01-22 |
| WO2008130552A1 (en) | 2008-10-30 |
| CN101663033B (en) | 2013-01-16 |
| EP2136803A1 (en) | 2009-12-30 |
| US7691887B2 (en) | 2010-04-06 |
| JP5498936B2 (en) | 2014-05-21 |
| EP2136803B1 (en) | 2012-05-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |